CN111544426A - 炔丙基半胱氨酸及其在制备新靶点药物中的用途 - Google Patents
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Abstract
本发明属生物医药领域，涉及炔丙基半胱氨酸及其在制备新靶点药物中的用途，尤其是用于制备治疗非酒精脂肪肝炎的药物中的用途；本发明所述的炔丙基半胱氨酸能直接结合靶点表皮生长因子受体(EGFR)及刺激其激活，进而降低非酒精性脂肪肝的血脂以及非酒精性脂肪肝引起的肝脏损伤；本发明所述的炔丙基半胱氨酸可用于制备预防和治疗非酒精脂肪肝和非酒精脂肪肝炎的药物。
Description
技术领域
本发明属生物医药领域，涉及炔丙基半胱氨酸及其在制备新靶点药物中的用 途，尤其是用于制备治疗非酒精脂肪肝炎的药物中的用途；本发明涉及的炔丙基 半胱氨酸可以直接结合表皮生长因子受体及刺激其激活，用于制备治疗非酒精脂 肪肝炎的药物。
背景技术
现有技术公开了炔丙基半胱氨酸是大蒜中的主要成分烯丙基半胱氨酸的结 构类似物；所述炔丙基半胱氨酸的初步药理学研究表明，其具有显著的心血管药 理活性，且具有潜在的药用价值；研究显示，炔丙基半胱氨酸还可发挥多种药理 药效作用，但这些药效作用靶点尚不甚明确，需要更进一步的研究探索及实验证 实。
研究公开了非酒精性脂肪肝炎是一种胰岛素拮抗和遗传易感密切相关的代 谢应激性肝脏损伤，是无大量饮酒且损伤可弥散在整个肝脏的一组疾病，临床实 践显示，该疾患以肝细胞脂肪变性和脂质储积为主要特征，易发展为肝硬化，且 与肝癌的发生有密切关系；还有研究显示，日常过多的高糖高脂饮食能导致肝脏 中脂肪的堆积并在非酒精性脂肪肝的发生过程中起到重要的作用。
基于现有技术的基础与现状，本发明拟提供炔丙基半胱氨酸在制备新靶点药 物中的用途，尤其是所涉及的炔丙基半胱氨酸通过直接结合表皮生长因子受体及 刺激其激活用于制备治疗非酒精脂肪肝炎的药物中的用途。
发明内容
本发明的目是基于现有技术的基础与现状，提供炔丙基半胱氨酸在制备新 靶点药物中的用途，尤其是在用于制备预防和治疗非酒精脂肪肝和非酒精脂肪肝 炎的药物中的用途；本发明所涉及的炔丙基半胱氨酸可以直接结合表皮生长因子 受体(EGFR)及刺激其激活，用于制备预防和治疗非酒精脂肪肝和非酒精脂肪 肝炎的药物。
本发明所述的非酒精性脂肪肝及非酒精性脂肪肝炎通常指由高糖高脂饮食 导致的非酒精性脂肪肝及非酒精性脂肪肝炎。
本发明中，提供并确定了式(I)的炔丙基半胱氨酸的一个新药物靶点为 表皮生长因子受体(EGFR)；所述表皮生长因子受体是一个跨膜糖蛋白，具有配 体诱导的酪氨酸蛋白激酶活性，所述的表皮生长因子受体是ErbB该保守的受体 家族的一个成员。
本发明通过实验证明了所述的炔丙基半胱氨酸通过激活所述的表皮生长因 子受体(磷酸化)产生预防与治疗非酒精性脂肪肝炎的作用：本发明中，所述的 炔丙基半胱氨酸作为药物活性成分，低浓度处理可以在分子及细胞水平激动所述 的表皮生长因子受体，产生有效的保护非酒精性脂肪肝及非酒精性脂肪肝炎的作 用。
本发明所述的非酒精脂肪肝和非酒精脂肪肝炎尤其指哺乳动物的非酒精性 脂肪肝和非酒精脂肪肝炎；所述哺乳动物特别指人。
本发明中，以所述的炔丙基半胱氨酸与所述的表皮生长因子受体蛋白进行分 子相互作用测试Biacore实验，结果显示，所述两者可以直接相互作用，同时， 本发明中通过计算机分子模拟实验预测炔丙基半胱氨酸可以与表皮生长因子受 体通过两个氢键相互作用。
本发明进一步进行了炔丙基半胱氨酸直接给药小鼠原代肝细胞试验，结果显 示，短时间所述炔丙基半胱氨酸内激活表皮生长因子受体；试验结果表明，炔丙 基半胱氨酸原料药物可以直接结合表皮生长因子受体(EGFR)并短时间内激动 该受体(磷酸化)从而发挥其药物机制；同时结果显示，炔丙基半胱氨酸给药可 以防止棕榈酸对肝细胞的损伤作用以及降低原代肝细胞对脂质的吸收；以及，炔 丙基半胱氨酸具有可降低非酒精性脂肪肝的血脂以及非酒精性脂肪肝引起的肝 脏损伤作用。
本发明提供了炔丙基半胱氨酸在制备新靶点药物中的用途，所述的炔丙基半 胱氨酸能直接结合靶点表皮生长因子受体(EGFR)及刺激其激活，进而降低非 酒精性脂肪肝的血脂以及非酒精性脂肪肝引起的肝脏损伤；本发明所述的炔丙基 半胱氨酸可用于制备治疗非酒精脂肪肝和非酒精脂肪肝炎的药物。
附图说明
图1:炔丙基半胱氨酸与表皮生长因子受体的直接相互作用，分子相互作用 测试。
图2:炔丙基半胱氨酸与表皮生长因子受体的计算机模拟相互作用方式。
图3：炔丙基半胱氨酸直接激活小鼠原代肝细胞中的表皮生长因子受体，同 时防止肝细胞被棕榈酸损伤以及产生降脂作用，其中，炔丙基半胱氨酸与棕榈酸 损伤组比较，*p<0.05。
具体实施方式
实施例1
采用炔丙基半胱氨酸与表皮生长因子受体(EGFR)蛋白进行分子相互作用 测试Biacore实验，用PBS溶解炔丙基半胱氨酸并制备浓度梯度溶液(78.125μM -625μM)，表皮生长因子受体50μg蛋白用PBS溶解后偶联至Biacore实验配 对芯片(CM5芯片)上，炔丙基半胱氨酸浓度梯度(78.125μM-625μM)经由 Biacore程序设定进针，实验结果显示，炔丙基半胱氨酸以浓度依赖性地发生直 接相互作用。
实施例2
采用计算机进行分子对接研究，进一步评估炔丙基半胱氨酸与表皮生长因子 受体之间的相互作用，结果显示，分子炔丙基半胱氨酸可以结合在野生型EGFR (PDB:2ITY)的活性位点中，如结合口袋表面图所示，SPRC(蓝色)与吉非替 尼(易瑞沙，粉红色)具有相似的方向，SPRC的氮原子位于吉非替尼的吲哚氮 原子的相同位置，其中预测NH和ASP 855之间的氢键具有相互作用；此外，SPRC 的羰基与LYS 745形成氢键，结果预测表明，SPRC可以在两个氢键的帮助下直 接靶向EGFR。
实施例3
采用胶原酶II配备肝脏消化液，用两步灌流消化法提取小鼠原代肝细胞并 铺板于培养板中，次日炔丙基半胱氨酸30μM直接处理小鼠原代肝细胞，结果 显示，15min短时间内激活表皮生长因子受体；400μM棕榈酸(10％BSA(W/L， 无脂肪酸)溶解于0.1M NaOH PBS配备棕榈酸母液，浓度为5mM，处理小鼠 原代肝细胞，结果显示，产生明显脂质储积以及肝细胞损伤，而炔丙基半胱氨酸 10～30μM处理则明显防止棕榈酸对肝细胞的损伤作用以及降低原代肝细胞对 脂质的吸收。
Claims (5)
1.式(Ⅰ)的炔丙基半胱氨酸在制备预防与治疗非酒精脂肪肝和非酒精脂肪肝炎的药物中的用途，
2.按权利要求1所述的用途，其特征在于，所述的药物中炔丙基半胱氨酸以表皮生长因子受体EGFR为靶点，所述的炔丙基半胱氨酸直接结合表皮生长因子受体EGFR及刺激其激活(磷酸化)，发挥其药物机制。
3.按权利要求1所述的用途，其特征在于，所述的预防与治疗非酒精脂肪肝和非酒精脂肪肝炎的药物为人的非酒精脂肪肝和非酒精脂肪肝炎的药物。
4.按权利要求1或3所述的用途，其特征在于，所述的非酒精性脂肪肝及非酒精性脂肪肝炎是由高糖高脂饮食导致的。
5.按权利要求2所述的用途，其特征在于，所述的药物机制是所述的炔丙基半胱氨酸直接结合表皮生长因子受体EGFR及刺激其激活，提高肝细胞活性从而防止脂肪肝状态下的肝细胞损伤以及降低肝细胞对脂质的吸收。
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112618531A (zh) * | 2019-10-08 | 2021-04-09 | 复旦大学 | 炔丙基半胱氨酸在制备受体激动制剂中的用途 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101932238A (zh) * | 2007-11-30 | 2010-12-29 | 加利福尼亚大学董事会 | 使用半胱胺制品治疗非酒精性脂肪性肝炎(nash)的方法 |
| KR20140086186A (ko) * | 2012-12-28 | 2014-07-08 | 한국식품연구원 | Ｓ-아릴 시스테인을 유효성분으로 함유하는 비만으로 유도된 염증 치료용 조성물 |
-
2019
- 2019-02-12 CN CN201910111434.1A patent/CN111544426A/zh active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101932238A (zh) * | 2007-11-30 | 2010-12-29 | 加利福尼亚大学董事会 | 使用半胱胺制品治疗非酒精性脂肪性肝炎(nash)的方法 |
| KR20140086186A (ko) * | 2012-12-28 | 2014-07-08 | 한국식품연구원 | Ｓ-아릴 시스테인을 유효성분으로 함유하는 비만으로 유도된 염증 치료용 조성물 |
Non-Patent Citations (4)
| Title |
|---|
| SHIGEKAZU TAKEMURA等: "S-Allyl cysteine improves nonalcoholic fatty liver disease in type 2 diabetes Otsuka Long-Evans Tokushima Fatty rats via regulation of hepatic lipogenesis and glucose metabolism", 《J CLIN BIOCHEM NUTR》 * |
| WENWEN LI等: "S-Propargyl-cysteine Exerts a Novel Protective Effect on Methionine and Choline Deficient Diet-Induced Fatty Liver via Akt/Nrf2/HO-1 Pathway", 《OXID MED CELL LONGEV》 * |
| YONG PIL HWANG等: "S-Allyl cysteine attenuates free fatty acid-induced lipogenesis in human HepG2 cells through activation of the AMP-activated protein kinase-dependent pathway", 《J NUTR BIOCHEM》 * |
| 严婧婷: "S-烯丙基半胱氨酸对大鼠非酒精性脂肪肝的影响以及机制研究", 《武汉科技大学硕士学位论文》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112618531A (zh) * | 2019-10-08 | 2021-04-09 | 复旦大学 | 炔丙基半胱氨酸在制备受体激动制剂中的用途 |
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